Core Modification of Cytisine: A Modular Synthesis

摘要

(-)-Cytisine (1) has occupied a pivotal role in nicotinic pharmacology as a partial agonist at the α4β2 subtype of neuronal nicotinic acetylcholine receptor (nAChR). More recently because of this partial agonist profile, cytisine provided the discovery lead for varenicline (2), Pfizer's smoking cessation agent which was launched in 2006.